ACS Medicinal Chemistry Letters · 2018 · 20 citations · 12 references
MedicineNeurosciencePharmacologyDrug DesignDrug DiscoveryNeuropharmacologyAmyotrophic Lateral SclerosisNeurodegenerative Disease PharmacologyNeurodegenerative Disease PharmacotherapyNeuroprotectionNeuroprotective PharmacologyEdaravone TherapyNeuroprotective AgentsNeuroprotective Drug DevelopmentNeuroprotective MechanismsNeuroprotective PharmacotherapyRiluzole TreatmentTriazole ChemistryTriazole Synthesis
Despite intense attention from biomedical and chemical researchers, there are few approved treatments for amyotrophic lateral sclerosis (ALS), with only riluzole (Rilutek) and edaravone (Radicava) currently available to patients. Moreover, the mechanistic basis of the activity of these drugs is currently not well-defined, limiting the ability to design new medicines for ALS. This Letter describes the synthesis of triazole-containing riluzole analogues, and their testing in a novel neuroprotective assay. Seven compounds were identified as having neuroprotective activity, with two compounds having similar activity to riluzole.
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Dendritic organization in the neurons of the visual and motor cortices of the cat.